EP2079307A4 - Agonistes du récepteur farnésoïde x - Google Patents

Agonistes du récepteur farnésoïde x

Info

Publication number
EP2079307A4
EP2079307A4 EP07863446A EP07863446A EP2079307A4 EP 2079307 A4 EP2079307 A4 EP 2079307A4 EP 07863446 A EP07863446 A EP 07863446A EP 07863446 A EP07863446 A EP 07863446A EP 2079307 A4 EP2079307 A4 EP 2079307A4
Authority
EP
European Patent Office
Prior art keywords
farnesoid
receptor agonists
agonists
receptor
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Granted
Application number
EP07863446A
Other languages
German (de)
English (en)
Other versions
EP2079307B1 (fr
EP2079307A2 (fr
Inventor
Jonathan York Bass Iii
David Norman Deaton
Justin Caravella
Robert Blount Mcfadyen
Frank Navas Iii
Paul Kenneth Spearing
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
GlaxoSmithKline LLC
Original Assignee
GlaxoSmithKline LLC
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by GlaxoSmithKline LLC filed Critical GlaxoSmithKline LLC
Publication of EP2079307A2 publication Critical patent/EP2079307A2/fr
Publication of EP2079307A4 publication Critical patent/EP2079307A4/fr
Application granted granted Critical
Publication of EP2079307B1 publication Critical patent/EP2079307B1/fr
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/02Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/06Antihyperlipidemics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Diabetes (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Pulmonology (AREA)
  • Dermatology (AREA)
  • Urology & Nephrology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
EP07863446.6A 2006-10-24 2007-10-23 Agonistes du récepteur farnésoïde x Active EP2079307B1 (fr)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US85388606P 2006-10-24 2006-10-24
US85533706P 2006-10-30 2006-10-30
US91195407P 2007-04-16 2007-04-16
PCT/US2007/082170 WO2008051942A2 (fr) 2006-10-24 2007-10-23 Agonistes du récepteur farnésoïde x

Publications (3)

Publication Number Publication Date
EP2079307A2 EP2079307A2 (fr) 2009-07-22
EP2079307A4 true EP2079307A4 (fr) 2010-09-15
EP2079307B1 EP2079307B1 (fr) 2013-07-17

Family

ID=39325319

Family Applications (1)

Application Number Title Priority Date Filing Date
EP07863446.6A Active EP2079307B1 (fr) 2006-10-24 2007-10-23 Agonistes du récepteur farnésoïde x

Country Status (6)

Country Link
US (2) US20100120775A1 (fr)
EP (1) EP2079307B1 (fr)
JP (1) JP5090458B2 (fr)
CL (1) CL2007003035A1 (fr)
ES (1) ES2428159T3 (fr)
WO (1) WO2008051942A2 (fr)

Families Citing this family (58)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2128158A1 (fr) 2008-05-26 2009-12-02 Phenex Pharmaceuticals AG Composés de liaison FXR substitués de cyclopropyle hétérocyclique
CA2744817C (fr) 2008-11-26 2020-07-07 Satiogen Pharmaceuticals, Inc. Inhibiteurs de recyclage de l'acide biliaire pour le traitement de l'obesite et du diabete
EP2379081B1 (fr) 2008-12-19 2013-03-20 Royal College of Surgeons in Ireland Traitement de la diarrhée
EP2289883A1 (fr) 2009-08-19 2011-03-02 Phenex Pharmaceuticals AG Nouveaux composés modulant l'activité du recepteur FXR (NR1H4)
CN102206187B (zh) * 2010-03-31 2013-01-02 北京大学 6-苄基-1-乙氧甲基-5-异丙基尿嘧啶及其类似物的合成方法
ES2552657T3 (es) 2010-05-26 2015-12-01 Satiogen Pharmaceuticals, Inc. Inhibidores del reciclado de ácidos biliares y saciógenos para el tratamiento de diabetes, obesidad, y afecciones gastrointestinales inflamatorias
EP2545964A1 (fr) 2011-07-13 2013-01-16 Phenex Pharmaceuticals AG Nouveaux composés se liant au fxr (nr1 h4) et modulant son activité
WO2013037482A1 (fr) 2011-09-15 2013-03-21 Phenex Pharmaceuticals Ag Agonistes du récepteur du farnésoïde x pour le traitement et la prévention du cancer
MX363161B (es) 2011-10-28 2019-03-13 Lumena Pharmaceuticals Inc Inhibidores de la recirculación de ácidos biliares para el tratamiento de hipercolemia y enfermedad hepática colestásica.
US20140243281A1 (en) 2011-10-28 2014-08-28 Lumena Pharmaceuticals, Inc. Bile acid recycling inhibitors for treatment of pediatric cholestatic liver diseases
JP5970245B2 (ja) * 2012-06-06 2016-08-17 公益財団法人ヒューマンサイエンス振興財団 幹細胞から肝細胞への分化誘導方法
CA3047776C (fr) * 2012-06-19 2022-10-18 Intercept Pharmaceuticals, Inc. Preparation, utilisations et formes solides d'acide obeticholique
CA2907214A1 (fr) 2013-03-15 2014-09-18 Lumena Pharmaceuticals, Inc. Inhibiteurs de recyclage d'acide biliaire pour le traitement de l'ƒsophage de barrett et du reflux gastroƒsophagien pathologique
KR20230152818A (ko) 2013-03-15 2023-11-03 샤이어 휴먼 지네틱 테라피즈 인크. 원발성 담관염 및 염증성 장 질환 치료용 담즙산 재순환 억제제
CN105764569B (zh) 2013-09-11 2019-09-13 国家医疗保健研究所 治疗乙型肝炎病毒感染的方法和药物组合物
US10077268B2 (en) 2014-03-13 2018-09-18 Salk Institute For Biological Studies FXR agonists and methods for making and using
US10301268B2 (en) 2014-03-13 2019-05-28 The Salk Institute For Biological Studies Analogs of fexaramine and methods of making and using
EP3006939A1 (fr) 2014-10-06 2016-04-13 Gilead Sciences, Inc. Glycoprotéine riche en histidine comme marqueur de l'activation du récepteur farnésoïde X hépatique
US10208081B2 (en) 2014-11-26 2019-02-19 Enanta Pharmaceuticals, Inc. Bile acid derivatives as FXR/TGR5 agonists and methods of use thereof
EP3034501A1 (fr) 2014-12-17 2016-06-22 Gilead Sciences, Inc. Hydroxy contenant des composés de modulation (FXR NR1H4)
EP3034499A1 (fr) 2014-12-17 2016-06-22 Gilead Sciences, Inc. Nouveaux composés de modulation (FXR NR1H4)
TW201628625A (zh) * 2015-02-06 2016-08-16 英特賽普醫藥品公司 組合療法醫藥組成物
TWI698430B (zh) 2015-02-13 2020-07-11 南北兄弟藥業投資有限公司 三環化合物及其在藥物中的應用
CN107530361A (zh) * 2015-03-09 2018-01-02 英特塞普特医药品公司 用于调节骨密度的方法
WO2016149111A1 (fr) * 2015-03-13 2016-09-22 Salk Institute For Biological Studies Traitement de diabètes auto-immuns latents des adultes à agonistes de récepteur x farnésoïde pour activer les récepteurs intestinaux
SI3277286T1 (sl) 2015-03-31 2021-09-30 Enanta Pharmaceuticals, Inc. Derivati žolčne kisline kot antagonisti FXR/TGR5 in metode za njihovo uporabo
EP3350166A4 (fr) * 2015-09-16 2019-05-01 Metacrine, Inc. Agonistes du récepteur x farnésoïde et leurs utilisations
WO2017189651A1 (fr) 2016-04-26 2017-11-02 Enanta Pharmaceuticals, Inc. Dérivés d'isoxazole utilisés comme agonistes de fxr et leurs méthodes d'utilisation
US10080743B2 (en) 2016-04-26 2018-09-25 Enanta Pharmaceuticals, Inc. Isoxazole derivatives as FXR agonists and methods of use thereof
WO2017189652A1 (fr) 2016-04-26 2017-11-02 Enanta Pharmaceuticals, Inc. Dérivés d'isoxazole utilisés comme agonistes de fxr et leurs procédés d'utilisation
WO2017201150A1 (fr) 2016-05-18 2017-11-23 Enanta Pharmaceuticals, Inc. Analogues de l'isoxazole comme agonistes de fxr et leurs procédés d'utilisation
US10138228B2 (en) 2016-05-18 2018-11-27 Enanta Pharmaceuticals, Inc. Isoxazole derivatives as FXR agonists and methods of use therof
WO2017201155A1 (fr) 2016-05-18 2017-11-23 Enanta Pharmaceuticals, Inc. Dérivés d'isoxazole utilisés comme agonistes de fxr et leurs méthodes d'utilisation
PL3730487T3 (pl) 2016-06-13 2022-08-16 Gilead Sciences, Inc. Pochodne azetydyny jako modulatory fxr (nr1h4)
CA2968836A1 (fr) 2016-06-13 2017-12-13 Gilead Sciences, Inc. Composes modulant fxr (nr1h4)
TW201808283A (zh) 2016-08-05 2018-03-16 廣東東陽光藥業有限公司 含氮三環化合物及其在藥物中的應用
CA3039124A1 (fr) 2016-10-04 2018-04-12 Enanta Pharmaceuticals, Inc. Analogues de l'isoxazole en tant qu'agonistes de fxr et leurs procedes d'utilisation
US10597391B2 (en) 2016-10-26 2020-03-24 Enanta Pharmaceuticals, Inc. Urea-containing isoxazole derivatives as FXR agonists and methods of use thereof
JP6906626B2 (ja) 2017-03-28 2021-07-21 ギリアード サイエンシーズ, インコーポレイテッド 肝疾患を処置するための治療的組み合わせ
US20210085662A1 (en) 2017-03-30 2021-03-25 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods and pharmaceutical compositions for reducing persistence and expression of episomal viruses
SG11201908235RA (en) 2017-04-12 2019-10-30 Il Dong Pharmaceutical Co Ltd An isoxazole derivatives as nuclear receptor agonists and used thereof
CN111630051B (zh) * 2017-11-01 2023-12-26 百时美施贵宝公司 作为法尼醇x受体调节剂的烯烃螺环化合物
JP7212693B2 (ja) 2017-11-01 2023-01-25 ブリストル-マイヤーズ スクイブ カンパニー ファルネソイドx受容体モジュレーターとしての架橋二環化合物
ES2944657T3 (es) 2017-11-01 2023-06-23 Bristol Myers Squibb Co Compuestos de alqueno como moduladores del receptor farnesoide X
WO2019089664A1 (fr) 2017-11-01 2019-05-09 Bristol-Myers Squibb Company Composés multicycliques en tant que modulateurs du récepteur farnésoïde x
WO2019118571A1 (fr) 2017-12-12 2019-06-20 Enanta Pharmaceuticals, Inc. Analogues de l'isoxazole utilisés en tant qu'agonistes de fxr et leurs procédés d'utilisation
CN110128432B (zh) 2018-02-02 2021-03-02 广东东阳光药业有限公司 含氮三环化合物及其在药物中的应用
WO2019160813A1 (fr) 2018-02-14 2019-08-22 Enanta Pharmaceuticals, Inc. Dérivés d'isoxazole en tant qu'agonistes de fxr et leurs procédés d'utilisation
AU2020209564B2 (en) 2019-01-15 2022-12-01 Gilead Sciences, Inc. FXR (NR1H4) modulating compounds
BR112021015799A2 (pt) 2019-02-12 2022-01-18 Mirum Pharmaceuticals Inc Métodos para aumentar o crescimento em pacientes pediátricos com doença colestática do fígado
AR118050A1 (es) 2019-02-15 2021-09-15 Bristol Myers Squibb Co Compuestos bicíclicos sustituidos como moduladores del receptor farnesoide x
JP2022519906A (ja) 2019-02-19 2022-03-25 ギリアード サイエンシーズ, インコーポレイテッド Fxrアゴニストの固体形態
WO2020231917A1 (fr) 2019-05-13 2020-11-19 Enanta Pharmaceuticals, Inc. Dérivés d'isoxazole utilisés en tant qu'agonistes de fxr et leurs procédés d'utilisation
CN114173784B (zh) 2019-07-18 2023-12-01 埃尼奥制药公司 降低干扰素的副作用的方法
EP4090327A1 (fr) 2020-01-15 2022-11-23 Institut National de la Santé et de la Recherche Médicale (INSERM) Utilisation d'agonistes de fxr pour traiter une infection par le virus de l'hépatite d
CA3204800A1 (fr) 2021-01-14 2022-07-21 Raphael Darteil Effet synergique d'un agoniste de fxr et d'ifn pour le traitement d'une infection par le virus de l'hepatite b
CN113185472B (zh) * 2021-04-12 2022-10-21 华南理工大学 一种合成4-烷氧基烯基异噁唑衍生物的方法
CA3213217A1 (fr) 2021-04-28 2022-11-03 Raphael Darteil Potentialisation forte d'effets d'agonistes de tlr3 a l'aide d'agonistes de fxr en tant que traitement combine

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Publication number Priority date Publication date Assignee Title
WO2007076260A2 (fr) * 2005-12-19 2007-07-05 Smithkline Beecham Corporation Agonistes de recepteur de farnesoide x

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AU2389100A (en) * 1998-12-23 2000-07-12 Glaxo Group Limited Assays for ligands for nuclear receptors
ATE283253T1 (de) 2000-09-18 2004-12-15 Glaxo Group Ltd Substituierte aminopropoxyarylderivate als lxr agonisten
ATE381542T1 (de) * 2001-08-13 2008-01-15 Phenex Pharmaceuticals Ag Nr1h4-kern-rezeptor-bindende verbindungen
US6987121B2 (en) * 2002-04-25 2006-01-17 Smithkline Beecham Corporation Compositions and methods for hepatoprotection and treatment of cholestasis
JP2006515838A (ja) * 2002-11-22 2006-06-08 スミスクライン ビーチャム コーポレーション ファルネソイドx受容体アゴニスト

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2007076260A2 (fr) * 2005-12-19 2007-07-05 Smithkline Beecham Corporation Agonistes de recepteur de farnesoide x

Also Published As

Publication number Publication date
EP2079307B1 (fr) 2013-07-17
US20100120775A1 (en) 2010-05-13
EP2079307A2 (fr) 2009-07-22
WO2008051942A3 (fr) 2008-07-03
WO2008051942A2 (fr) 2008-05-02
CL2007003035A1 (es) 2008-05-16
US20080096921A1 (en) 2008-04-24
US7960552B2 (en) 2011-06-14
JP5090458B2 (ja) 2012-12-05
ES2428159T3 (es) 2013-11-06
JP2010507684A (ja) 2010-03-11

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